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SKF 89976A hydrochloride

Cat. No. M1891
SKF 89976A hydrochloride Structure
Size Price Availability Quantity
10mg USD 120 In stock
50mg USD 440 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

SKF 89976A hydrochloride is a potent inhibitor of GABA uptake with IC50 of 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively. GABA transporter subtype 1 (GAT-1) and GABA transporter subtype 3 (GAT-3) are the main transporters that regulate inhibitory GABAergic transmission in the mammalian brain through GABA reuptake. GAT-1 inhibitor SKF 89976A significantly prolonged the decay time, but did not affect the amplitude, of eIPSCs induced by striatal stimulation (15-20 V). Furthermore, SKF 89976A blockade also increased the amplitude and frequency of spontaneous IPSCs, but did not affect miniature IPSCs. SKF 89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). In vivo, SKF 89976A is able to pass the blood-brain barrier after systemic administration and is active.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 371.91
Formula C22H25NO2.HCl
CAS Number 85375-15-1
Purity >99%
Solubility DMSO
Water
Storage at -20°C
References

Differential localization and function of GABA transporters, GAT-1 and GAT-3, in the rat globus pallidus.
Jin XT, et al. Eur J Neurosci. 2011 Apr;33(8):1504-18. PMID: 21410779.

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  Catalog
Abmole Inhibitor Catalog 2017




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